OXYTOCIN-ANALOGA, IHRE HERSTELLUNG UND PHARMAZEUTISCHE MITTEL

• Main Authors: HRBAS,PAVEL,DR, BARTH,TOMISLAV,DR, SKOPKOVA,JANA,DR, LEBL,MICHAL, MACHOVA,ALENA,DR, SLANINOVA,JIRINA,DR, JOST,KAREL,DR
• Format: Patent
• Language: German
• Published: 08.04.1982
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

Analogs of oxytocin of general formula I where all amino acids are L-isomers and X is phenylalanine or phenylalanine substituted in the p-position by alkyl, ethoxy, amino, substituted amino, or nitro group, suitable for medical applications, and a method for their preparation consisting in the cyclization of linear octapeptides of general formula II where X has the aforesaid meaning and Act is a group activating the carboxylic group of S-carboxyethylhomocysteine residue, e.g. an active ester. Two methods may be used for the preparation of [2-p-aminophenylalanine] deamino-6-carba-oxytocin, either the reduction of [2-p-nitrophenylalanine]- deamino-6-carba-oxytocin or deprotection of [2-p- benzyloxycarbonylaminophenylalanine] deamino-6-carba-oxytocin.